Plasma and Blood Stability
The measurement of the stability of a new chemical entity in a matrix such as plasma helps in identifying and understanding the lability of known structural moieties (e.g. amides, sulphonamide, esters, lactones and lactams to name a few) in molecules in the prioritisation of these for in vivo PK studies. High instability can result in aberrant PK results due to high clearance and short half-lives. Species differences in plasma stability for molecules is not uncommon and should be determined.
Sygnature’s plasma stability assay measures the stability of molecules in mouse, rat and human plasma (please enquire about other species). The molecule to be tested and controls (positive and negative) are incubated with plasma for a defined period and the percent remaining and half-life determined.
Propantheline (human), Enalapril (mouse and rat), Vinpocetin (rat) and/or Benfluorex (human and rat) are included as positive control compounds. Pepstatin or Leupeptin are included as negative controls.
For more information on microsomal metabolic stability and its impact, you can visit Sygnature Discovery’s technical note: Microsomal Metabolic Stability.